Richter Gedeon Vegyeszeti Gyar Rt

Egis Gyogyszergyar

Janos Brlik

Ferenc Trischler

Zoltan Tuba

Gabor Gigler

Frigyes Gorgenyi

Jozsef Reiter

Pal Fekete

Peter Tompe

Margit Csorgo

Adam Demeter

Eva Szabo

Maria Kiraly Nee Ignacz

Ilona Sztruhar

Janos Szeles

Peter Slegel

Gabriella Szilagyi

Erika Bakcsi

Janos Horvath

Adam Bor

György Galik

Bela Sörös

Agnes Halbauer Nee Nagy

Magdolna Kenyeres Nee Feher

Sarolta Benko Nee Markus

Szvetlana Zsarnoczai Nee Kurnyecova

Dezso Danyi

A new process is disclosed for the synthesis of racemic or optically pure N-[4-cyano-3-trifluoro-methyl-phenyl]-3[4-fluorophenyl-sulfonyl]-2-hydroxy-2-methylpropionamide. The process includes the formation of several novel intermediates in the synthesis.

Process for the synthesis of N-(4-cyano-3-trifluoromethylphenyl)-3-(4-fluorophenylsulfonyl)-2-hydroxy-2-methylpropionamide

Process for the synthesis of a-nor-seco compounds with sterane skeleton

This invention relates to a new and improved process for the preparation of 6,7-dichloro-1,5-dihydroimidazo[2,1-b]-quinazolin-2[3H]-one of formula ##STR1## (anagrelide), a valuable blood platelet antiaggregative compound. According to the process of the invention the compound of formula (I) is prepared by subjecting a new 2-cyanoiminoquinazoline derivative of the general formula ##STR2## wherein R stands for cyano or a group of the formula COOR.sup.1, in the latter R.sup.1 representing lower alkyl optionally carrying a phenyl substituent, to thermal cyclization in an acidic medium. The invention also relates to new 2-cyanoiminoquinazo-lines of the general formula (III) used for the production of anagrelide and to the preparation of the said compounds. The invention provides an advantageous process for the preparation of anagrelide which is devoid of the drawbacks of the hitherto known processes and renders possible the production of the compound of the formula (I) on industrial scale, too.

Process for the preparation of

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Budapest, Hungary

Janos Brlik